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Imidazole derivatives are important heterocyclic pharmacophores in medicinal chemistry, well known for their broad spectrum of biological activities and therapeutic potential.1 In agricultural applications they target cholinesterases (acetylcholinesterase, AChE and butyrylcholinesterase, BuChE), which are important for the normal function of the nervous system in humans, other vertebrates and insects. Consequently, dual evaluation AChE and BuChE inhibition characterizes the potency, selectivity, and toxicological safety of newly synthesized imidazoles as agrochemicals.2
In this work, a series of novel alkylamide derivatives of 1H-imidazole-4-carboxylic acid were synthesized using a modified Steglich EDC × HCl/DMAP amidation method under mild reaction conditions. Structural modifications included the incorporation of selected aliphatic amines in order to investigate structure–activity relationships. All compounds were characterized by melting point determination, 1H and 13C NMR spectroscopy, and mass spectrometry. To achieve a comprehensive understanding of their cholinesterase inhibition profiles, the synthesized derivatives were screened for dual inhibitory activity against AChE and BuChE.
Keywords: acetylcholinesterase, butyrylcholinesterase, imidazole, 1H-imidazole-4-carboxylic acid
References:
1. Bendi, A; Vashisth, C; Devi, P; Bhathiwal, AS; Pundeer, R; Mittal, C; Raghav, N; Afshari, M. From Lab to Life: The Journey of imidazoles Through Advanced Synthesis and Vital Biological Applications (Comprehensive Review). ChemistrySelect. 2025, 10, e202500631. https://doi.org/10.1002/slct.202500631
- Karnaš, M; Rastija, V; Šubarić, D; Molnar, M. Green Synthesis and Acetylcholinesterase Inhibition of Coumarin-1,2,4-Triazole Hybrids. Curr. Org. Chem. 2023, 27, 883–892. https://doi.org/10.2174/1385272827666230817145725